An inhibitor of PI3KαH1047R
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RLY-2608

Item No. 44472

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano[1,2,4] triazolo[1,5-a]pyridin-6-yl)-2,3-dihydro-1-oxo-1H-isoindol-4-yl]-3-fluoro-5-(trifluoromethyl)-benzamide
CAS Number
2733573-94-7
Molecular Formula
C29H14ClF5N6O2
Formula Weight
608.9
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
FC1=CC([C@@H]2NC(C3=CC(C4=C(C#N)N5N=CN=C5C=C4)=CC(NC(C6=CC(C(F)(F)F)=CC(F)=C6)=O)=C32)=O)=C(Cl)C=C1
InChi Code
InChI=1S/C29H14ClF5N6O2/c30-21-3-1-16(31)10-19(21)26-25-20(28(43)40-26)7-13(18-2-4-24-37-12-38-41(24)23(18)11-36)8-22(25)39-27(42)14-5-15(29(33,34)35)9-17(32)6-14/h1-10,12,26H,(H,39,42)(H,40,43)/t26-/m0/s1
InChi Key
VYWRYBZVVSPTQN-SANMLTNESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $185

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    10 mg

    $308

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    25 mg

    $564

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    Product Description

    RLY-2608 is an inhibitor of PI3Kα containing a histidine-to-arginine mutation at position 1,047 (PI3KαH1047R; IC50 = 4 nM).1 It is selective for PI3KαH1047R over wild-type PI3Kα (IC50 = 48 nM). RLY-2608 (25 and 100 mg/kg) reduces tumor volume in T47D and ST1056 PI3KαH1047R mutant-containing breast cancer mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Varkaris, A., Pazolli, E., Gunaydin, H., et al. Discovery and clinical proof-of-concept of RLY-2608, a first-in-class mutant-selective allosteric PI3Kα inhibitor that decouples antitumor activity from hyperinsulinemia. Cancer Discov. 14(2), 240-257 (2024).